Synthesis of novel pleuromutilin derivatives. Part 1: Preliminary studies of antituberculosis activity

摘要

The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 mu M, with a MIC of one of the analogues as low as 7.2 mu M. (C) 2015 Elsevier Ltd. All rights reserved.